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001-es BibID:	BIBFORM120781
035-os BibID:	(Scopus)85190140338 (WOS)001200201600001
Első szerző:	Moreau, François
Cím:	Potentiating Activity of GmhA Inhibitors on Gram-Negative Bacteria / François Moreau, Dmytro Atamanyuk, Markus Blaukopf, Marek Barath, Mihály Herczeg, Xavier Nuno M., Monbrun Jérôme, Airiau Etienne, Henryon Vivien, Leroy Frédéric, Floquet Stéphanie, Bonnard Damien, Szabla Robert, Brown Chris, Junop Murray S., Kosma Paul, Gerusz Vincent
Dátum:	2024
ISSN:	0022-2623 1520-4804
Megjegyzések:	Inhibition of the biosynthesis of bacterial heptoses opens novel perspectives for antimicrobial therapies. The enzyme GmhA responsible for the first committed biosynthetic step catalyzes the conversion of sedoheptulose 7- phosphate into D-glycero-D-manno-heptose 7-phosphate and harbors a Zn2+ ion in the active site. A series of phosphoryl- and phosphonyl-substituted derivatives featuring a hydroxamate moiety were designed and prepared from suitably protected ribose or hexose derivatives. High-resolution crystal structures of GmhA complexed to two N-formyl hydroxamate inhibitors confirmed the binding interactions to a central Zn2+ ion coordination site. Some of these compounds were found to be nanomolar inhibitors of GmhA. While devoid of HepG2 cytotoxicity and antibacterial activity of their own, they demonstrated in vitro lipopolysaccharide heptosylation inhibition in Enterobacteriaceae as well as the potentiation of erythromycin and rifampicin in a wild-type Escherichia coli strain. These inhibitors pave the way for a novel treatment of Gram-negative infections.
Tárgyszavak:	Természettudományok Kémiai tudományok idegen nyelvű folyóiratközlemény külföldi lapban folyóiratcikk Gram-Negative GmhA Inhibitors D-glycero-D-manno-heptose antibacterial activity lipopolysaccharide
Megjelenés:	Journal Of Medicinal Chemistry. - 67 : 8 (2024), p. 6610-6623. -
További szerzők:	Atamanyuk, Dmytro Blaukopf, Markus Barath, Marek Herczeg Mihály (1979-) (vegyész, biológia-kémia tanár) Xavier, Nuno M. Monbrun, Jérôme Airiau, Etienne Henryon, Vivien Leroy, Frédéric Floquet, Stéphanie Bonnard, Damien Szabla, Robert Brown, Chris Junop, Murray S. Kosma, Paul Gerusz, Vincent
Internet cím:	Szerző által megadott URL DOI Intézményi repozitóriumban (DEA) tárolt változat
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